Pharmacotherapy of opioids: present and future developments

Abstract

The clinically available opioids have different physicochemical properties, resulting in differences in clinical profile with regard to potency, onset, and duration of activity. However, they all have comparable side-effects after acute systemic application. Several approaches can be used to overcome these side-effects. The following approaches, with special emphasis on the perioperative use of the opioids, are discussed: (1) the use of alternative routes of administration, such as via the spine (epidurally and intrathecally); (2) optimization of opioid delivery by means of slow-release preparations, chronic infusions with indwelling catheters, and transdermal delivery systems; (3) use of additional agents to potentiate the analgesic properties of the opioids so that the dose of opioid can be reduced; and (4) searching for new analgesics on the basis of knowledge of the pain-transmission system and the different opioid receptors with their functional interactions.

Sufentanil–2‐Hydroxypropyl‐β‐Cyclodextrin Inclusion Complex for pain Treatment: Physicochemical, Cytotoxicity, and Pharmacological Evaluation

“…In this study, we provided detailed information about physicochemical characterization including cytotoxic assays in combination with pharmacological evaluation by intramuscular administration, in a different manner of those previous studies. As SUF is rapidly absorbed after intramuscular injection and is effective at low concentrations,2 these features point out the complex as a potential new formulation to enhance the analgesic effects of this drug, being advantageous for the treatment of pain by intramuscular administration.…”

“…However, constant rate infusions or repeated injections are often used to overcome the short duration of action, evoking typical opioid side effects such as, bradycardia, respiratory depression, or excessive sedation. In the light of these observations, SUF was selected for this study because of its high potency and effective release after intramuscular injection,1,2 being an interesting molecule for the development of drug‐delivery systems for opioid analgesics.…”

A comparison between pre-operative carprofen and a long-acting sufentanil formulation for analgesia after ovariohysterectomy in dogs

“…These systems can be produced by forming suspensions, gels, emulsions, liposome dispersions or micro emulsions. Sufentanil is rapidly absorbed after IM injection and is effective at low concentrations (Meert 1996) making it an ideal candidate for a sustained‐release formulation (Lee & Putnam 2000). The actual technique for producing the long‐acting sufentanil used in this study is currently not publicly available but liposome encapsulation has been used to produce sustained release formulations of both morphine (Howell 2001) and oxymorphone (Smith et al.…”

Comparison of two automated solid phase extractions for the detection of ten fentanyl analogs and metabolites in human urine using liquid chromatography tandem mass spectrometry

“…It is important to note that the common nor-metabolites are not unique to each fentanyl analog; therefore, to correctly identify the exposure agent, the native compound of all suspected fentanyls must be also monitored, (e.g. sufentanil and alfentanil both metabolize to the metabolite norsufentanil) [10-12]. …”